IP Library Granted Patent US 8,710,100
Granted Patent B2
US 8,710,100 · App. 13/408,439 · Granted Apr 29, 2014

Compounds and their salts specific to the PPAR receptors and the EGF receptors and their use in the medical field

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,710,100
App. No.
13/408,439
Granted
Apr 29, 2014
Kind
B2
Abstract

The present invention relates to compounds comprising the general formula (I), in which R 1 and R 2 , which may be identical or different, are selected from the group comprising —H or a linear or branched alkyl group having from 1 to 6 carbon atoms or together form an aromatic or aliphatic ring with 5 or 6 atoms; Y and Z, which may be identical or different, are selected from the group comprising —H, —OH, —COOH, —OR 3 , —CH(OR 3 )COOH, in which R 3 is selected from H, phenyl, benzyl, —CF 3 or —CF 2 CF 3 , vinyl, allyl and a linear or branched alkyl group having from 1 to 6 carbon atoms.

Claims (15)

1. A method of treating Crohn's disease or ulcerative rectocolitis, comprising administering to a mammal in need thereof a compound that activates a PPARγ receptor, and represented by the general formula (I)

in which

R 1 and R 2 , which may be identical or different, are selected from the group consisting of —H or a linear or branched alkyl group having from 1 to 6 carbon atoms;

Y is selected from the group consisting of —H, —OH, —OR 3 , or —COOH wherein R 3 is selected from the group consisting of phenyl, benzyl, —CF 3 , —CF 2 CF 3 , vinyl, allyl, and a linear or branched alkyl group having from 1 to 6 carbon atoms;

Z is —CH(OR 3 )COOH, in which R 3 is selected from the group consisting of H, phenyl, benzyl, —CF 3 or —CF 2 CF 3 , vinyl, allyl and a linear or branched alkyl group having from 1 to 6 carbon atoms; or salts thereof.

2. The method of claim 1 , wherein the mammal is a human.

3. The method of claim 1 , wherein Y is H.

4. The method of claim 1 , wherein Z is —CH(OR 3 )COOH, wherein R 3 is selected from the group consisting of —CH 3 or —CH 2 CH 3 .

5. A method of treating Crohn's disease in a patient in need thereof, comprising administering an effective amount of a compound having PPARγ receptor activity, wherein the compound is selected from the group consisting of:

6. The method of claim 1 , wherein the compound is selected from the group consisting of: ±−2-methoxy-3-(3′-aminophenyl)propionic acid and ±−2-methoxy-3-(4′-aminophenyl)propionic acid.

7. The method of claim 1 , wherein the chronic inflammatory disease is Crohn's disease.

8. The method of claim 1 , wherein the chronic inflammatory disease is ulcerative rectocolitis.

9. A method of treating Crohn's disease in a mammal in need thereof, comprising administering to said mammal a compound having PPARγ receptor activity, wherein the compound is represented by:

or salts thereof.

10. The method of claim 9 , wherein the compound is in an enantiomerically pure R or S form.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 25, 2013
From: NACCARI, GIANCARLO; BARONI, SERGIO
To: GIULIANI INTERNATIONAL LIMITED
Reel/Frame 030879/0079 →
CHANGE OF NAME Recorded Nov 14, 2012
From: GIULIANI INTERNATIONAL LIMITED
To: NOGRA PHARMA LIMITED
Reel/Frame 029295/0861 →